Synthesis and evaluation of new pyrazoline-thiazole derivatives as monoamine oxidase inhibitors

ACAR ÇEVİK U., OSMANİYE D., SAĞLIK B. N., LEVENT S., KAYA ÇAVUŞOĞLU B., ÖZKAY Y., ...Daha Fazla

JOURNAL OF HETEROCYCLIC CHEMISTRY, cilt.56, sa.11, ss.3000-3007, 2019 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 56 Sayı: 11
  • Basım Tarihi: 2019
  • Doi Numarası: 10.1002/jhet.3694
  • Dergi Adı: JOURNAL OF HETEROCYCLIC CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.3000-3007
  • Anadolu Üniversitesi Adresli: Evet

Özet

A novel series of 1,3,5-trisubstituted-2-pyrazoline derivatives (4a-4k) was synthesized and their chemical structures characterized by H-1 NMR, C-13 NMR, and mass spectroscopy. These compounds were evaluated as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes. The most common inhibitors of MAO enzymes used to treat depression and anxiety such as selegiline and moclobemide drugs were used as reference agents. A result of biological evaluation of these compounds revealed compounds 4c, 4d, and 4i as potent and selective MAO A inhibitors. The most active compound 4i, which is 2,4-dimethoxy at phenyl ring, showed strong inhibitory activity at MAO A (IC50 of 0.0445 +/- 0.0018 mu M). Furthermore, compounds 4c and 4d showed significant inhibition profile on MAO A with the IC50 values 0.1423 +/- 0.0051 mu M and 0.2148 +/- 0.0067 mu M, respectively.